Cancer, also known as a malignant tumor, is a group of diseases involving abnormal cell growth with the potential to invade or spread to other parts of the body. In 2012 about 14.1 million new cases of cancer occurred globally, which caused about 8.2 million deaths or 14.6% of all human deaths. Development of prevention and treatment of cancer drugs will bring benefits to mankind, is of great significance. The important feature of tumor cells is abnormal differentiation, not starting the normal process of apoptosis.
Millettia pachycarpa is a perennial climbing shrub belonging to the genus Millettia. It is named as Houguojixueteng in Chinese, mainly distributing in Sichuan, Yunnan, Guangdong, Guangxi and Guizhou province in China and is widely used as an antihelminthic, a medication capable of causing the evacuation of parasitic intestinal worms. M. pachycarpa is well known to be a rich reservoir of bioactive flavonoids, which exhibited various biological activities including anti-inflammatory, anti-tumor, anti-allergic, anti-microbial and significant cytotoxic effects. Millepachine ((E)-1-(5-methoxy-2,2-dimethyl-2H-chromen-8-yl)-3-(4-methoxyphenyl)prop-2-en-1-one) was isolated as active principles from Chinese herbal medicine M. pachycarpa Benth. The novel chalcone was then evaluated for cytotoxic effects against several cancer cell lines. And its apoptosis-inducing effect was tested against HeLa-C3 cells. Both studies showed that millepachine demonstrated significant cytotoxic and apoptotic effects against cancer cells. As a part of continuing search for novel anticancer agents, a series of novel millepachine derivatives have been designed, synthesized and evaluated for antitumor activity by MTT assay.